PF-998425

PF-998425 is a potent, selective nonsteroidal androgen receptor (AR) antagonist with an IC₅₀ of 37 nM and 43 nM in AR binding and cellular assays, respectively. PF-998425 has low activity on common receptors and enzymes, such as progesterone receptor. PF-998425 can be used for sebum control and androgenetic alopecia research^[1]. IC50 & Target:IC50: 37 nM (AR binding) and 43 nM (AR cellular)^[1] In Vivo: PF-998425 (Compound (-)-6a) is rapidly metabolized in rat liver microsomes (t_1/2=4 min, C_Lint=350 (µL/min)/mg protein). In vivo clearance data in dogs are consistent with the high clearance predicted in vitro in rat. Following intravenous administration of PF-998425, mean systemic plasma clearance is 40 (mL/min)/kg. The mean apparent of volume of distribution at steady state is 6.5 L/kg, and the mean terminal phase half-life is 2.6 h^[1].